Tramadol hydrochloride (trademarked
as Conzip, Ryzolt, Ultracet, Ultram in the USA, Ralivia and Zytram XL in
Canada) is a centrally-acting synthetic analgesic used to treat moderate to
moderately-severe pain. The drug has a wide range of applications, including
treatment of rheumatoid arthritis, restless legs syndrome and fibromyalgia. It
was launched and marketed as Tramal by the German pharmaceutical company
Grünenthal GmbH in 1977.
Tramadol is a very weak μ-opioid
receptor agonist, induces serotonin release, and inhibits the reuptake of
norepinephrine. Tramadol is converted to O-desmethyltramadol, a significantly
more potent μ-opioid agonist. The opioid agonistic effect of tramadol and its
major metabolite(s) is almost exclusively mediated by such μ-opioid receptors.
This further distinguishes tramadol from opioids in general (including
morphine), which do not possess tramadol's degree of receptor subtype
selectivity and which are much stronger opiate-receptor agonists. Similarly,
the habituating properties of tramadol (such as they are) are arguably mainly
due to μ-opioid agonism with contributions from serotonergic and noradrenergic
effects.
Clinical data
Trade names Ryzolt,
Ultram
AHFS/Drugs.com monograph
MedlinePlus a695011
Pregnancy cat. C (AU)
C (US)
Legal status Prescription
Only (S4) (AU) POM (UK) ℞-only (US) ℞
Prescription only
Routes Oral, IV, IM,
rectal, sublingual, buccal, intranasal
Pharmacokinetic data
Bioavailability 68–72%(Increases
with repeat dosing.)
Protein binding 20%
Metabolism Hepatic
demethylation and glucuronidation
Half-life 5.5–7
hours
Excretion Renal
Identifiers
CAS number 27203-92-5
ATC code N02AX02
PubChem CID
33741
DrugBank DB00193
ChemSpider 31105
UNII 39J1LGJ30J
KEGG D08623
ChEMBL CHEMBL1066
Chemical data
Formula C16H25NO2
Mol. mass 263.4
g/mol
No comments:
Post a Comment